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Medicines 2016, 3(4), 30; doi:10.3390/medicines3040030

Identification of Phlogacantholide C as a Novel ADAM10 Enhancer from Traditional Chinese Medicinal Plants

1
Clinic of Psychiatry and Psychotherapy, University Medical Center of the Johannes Gutenberg-University Mainz, 55131 Mainz, Germany
2
Institute of Pharmacy, Johannes Gutenberg-University Mainz, 55099 Mainz, Germany
*
Author to whom correspondence should be addressed.
Academic Editor: James D. Adams
Received: 18 October 2016 / Revised: 14 November 2016 / Accepted: 28 November 2016 / Published: 5 December 2016
(This article belongs to the Special Issue Herbal Medicines and Functional Foods)
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Abstract

Background: Alzheimer’s disease is one of the most prevalent dementias in the elderly population with increasing numbers of patients. One pivotal hallmark of this disorder is the deposition of protein aggregates stemming from neurotoxic amyloid-beta peptides. Synthesis of those peptides has been efficiently prevented in AD model mice by activation of an enzyme called alpha-secretase. Therefore, drugs with the capability to increase the expression of this enzyme, named ADAM10, have been suggested as a valuable therapeutic medication. Methods: We investigated 69 substances from a drug library derived from traditional Chinese medicine by luciferase reporter assay in human neuronal cells for their potential to selectively induce alpha-secretase expression. Western blot analysis was used to confirm results on the protein level. Results: Ten of the 69 investigated compounds led to induction of ADAM10 transcriptional activity while BACE-1 (beta-site APP cleaving enzyme 1) and APP (amyloid precursor protein) expression were not induced. Two of them—Norkurarinol and Phlogacantholide C—showed substantial elevation of ADAM10 protein levels and Phlogacantholide C also increased secretion of the ADAM10-derived cleavage product APPs-alpha. Conclusion: Phlogacantholide C represents a novel ADAM10 gene expression enhancer from traditional Chinese medicinal herbs that may lay the groundwork for evolving potential novel therapeutics in Alzheimer’s disease. View Full-Text
Keywords: ADAM10; Amyloid precursor protein; Alzheimer’s disease; Norkurarinol; Phlogacantholide C; Phlogacanthus curviflorus; Sophora flavescens ADAM10; Amyloid precursor protein; Alzheimer’s disease; Norkurarinol; Phlogacantholide C; Phlogacanthus curviflorus; Sophora flavescens
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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MDPI and ACS Style

Meineck, M.; Schuck, F.; Abdelfatah, S.; Efferth, T.; Endres, K. Identification of Phlogacantholide C as a Novel ADAM10 Enhancer from Traditional Chinese Medicinal Plants. Medicines 2016, 3, 30.

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